[3][1] Proxicromil was developed in the late 1970s as an oral analogue and a successor of anti-allergy drug Intal, whose patent protection period was to expire in 1982.

Disodium cromoglycate in the form of an inhaler licensed as Intal (derived from ‘interfere with allergy’) had become the Fisons company's leading product, generating immense income and stimulating further research; thus several attempts at developing a congener were undertaken.

Antimicrobial cytotoxic and inflammatory mediators, such as histamine, proteoglycans, serotonin and serine proteases, are released from cytoplasmic granules in the mast cells once their high-affinity receptors FcεRI detect IgE antibodies and bind their Fc region.

[2] Proxicromil acts as an inhibitor of this process, competing with IgE antibodies for binding with the FcεRI receptors, thereby reducing the irritation caused by histamines.

Furthermore, the antihistamine blocks the elicitation of adoptively transferred EAE, an allergic brain inflammation reaction, and it shows a reducing effect on the severity of skin irritation.

[7][3] The pathway of metabolism, by most tested species, is by hydroxylation of the alicyclic ring to yield monohydroxylated metabolites with trace amounts of dihydroxylated product.

The reason for this difference in species, results from the dog having a higher dependence on biliary excretion of the unchanged drug for clearance.

[8] Proxicromil is tested through a variety of independent studies for its beneficial effect as an anti-allergen, its efficacy against migraine, asthma and tumor enhancement.

This comes through the route of excretion which Proxicromil undergoes and which leads to a high concentrations at the biliary canaliculus and thus its accumulation and a consequent increase in hepatic exposure.